Development of raloxifene-solid dispersion with improved oral bioavailability via spray-drying technique

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Raloxifene (RXF) is a selective estrogen receptor modulator with limited oral bioavailability.
• Enhancing RXF's dissolution rate and bioavailability is crucial for effective therapeutic outcomes.
• Solid dispersion technology offers a promising approach to overcome poor drug solubility.

Purpose of the Study:

• To develop a raloxifene-loaded solid dispersion using spray-drying.
• To enhance the dissolution rate and oral bioavailability of raloxifene.
• To evaluate the in vivo performance of the developed solid dispersion.

Main Methods:

• Preparation of raloxifene-loaded solid dispersions with PVP K30 at various weight ratios (1:4, 1:6, 1:8) via spray-drying.
• Characterization using differential scanning calorimetry, X-ray powder diffraction, and scanning electron microscopy.
• In vitro solubility and dissolution testing, followed by in vivo bioavailability studies in rats.

Main Results:

• The spray-dried solid dispersion exhibited an amorphous form of raloxifene.
• Significant increases in solubility and dissolution rate were observed for the solid dispersion.
• In vivo studies showed a 2.6-fold enhancement in bioavailability compared to pure raloxifene.
• The solid dispersion demonstrated bioequivalence to a commercial raloxifene product in rats.

Conclusions:

• Amorphous solid dispersion of raloxifene prepared by spray-drying effectively enhances its oral bioavailability.
• This formulation strategy presents a viable option for improving raloxifene's therapeutic efficacy.
• The developed solid dispersion is comparable to existing commercial products in terms of pharmacokinetic parameters.